Necroptosis

Necroptosis is a form of regulated necrotic cell death mediated by receptor-interacting serine-threonine kinase 3 (RIPK3) and mixed lineage kinase domain-like (MLKL) and generally manifests with morphological features of necrosis. Necroptosis is characterized by early loss of plasma membrane integrity, leakage of intracellular contents, and organelle swelling. The cells dying through necroptosis lack the typical apoptotic characteristics, such as membrane blebbing, chromatin condensation, and intranucleosomal DNA cleavage into 180 bp DNA laddering, but may show TUNEL positivity.

Necroptosis triggers innate immune responses by rupturing dead cells and releasing intracellular components, it can be caused by Toll-like receptor (TLR)-3 and TLR-4 agonists, tumor necrosis factor (TNF), certain microbial infections, and T cell receptors. Necroptosis signaling is modulated by receptor-interacting protein kinase (RIPK) 1 when the activity of caspase-8 becomes compromised. Activated death receptors (DRs) cause the activation of receptor-interacting serine-threonine kinase 1 (RIPK1) and the RIPK1 kinase activity-dependent formation of an RIPK1-RIPK3-MLKL, which is complex II. RIPK3 phosphorylates MLKL, ultimately leading to necrosis through plasma membrane disruption and cell lysis.

Necroptosis Related Products (117):

By Effects:	Control (1) Inhibitors (46) Activators (3) Inducers (59)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-162097

RIPK1-IN-20	Inhibitor
RIPK1-IN-20 (compound 13c) has a favorable RIPK1 kinase inhibition activity with an IC₅₀ value of 59.8 nM. RIPK1-IN-20 blocks TNFα-induced necroptosis in both human and murine cells (EC₅₀=1.06–4.58 nM).

HY-175030

TNI-97	Inducer
TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC₅₀ of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.

HY-B1984S

p,p'-DDD-d₈	Inducer
p,p'-DDD-d₈ is the deuterium labeled p,p'-DDD[1]. p,p'-DDD (4,4’-DDD) is an organochlorine insecticide, a major metabolite of p,p'-DDT. p,p'-DDD is an agonist at estrogen receptor α(ERα) and ERβ. p,p'-DDD increases DNA damage, apoptosis and necrosis in peripheral blood. p,p'-DDD stimulates cell proliferation in SKBR3 cells. p,p'-DDD activates the AP-1 transcription factor. p,p'-DDD decreases sleep times of barbiturates and steroids in rats.

HY-B0863S5

Glyphosate-¹³C,¹⁵N-1
Glyphosate-¹³C,¹⁵N-1 is the ¹³C- and ¹⁵N-labeled Glyphosate (HY-B0863). Glyphosate, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders.

HY-N10520

Pectic acid	Inducer
Pectic acid (Methyl protopectin), a polygalacturonic acid, induces cell apoptosis and necrosis in pituitary tumor cells. Pectic acid can be used in the research of cancers and autoimmune disease.

HY-144277

RIPK1-IN-12	Inhibitor
RIPK1-IN-12 is a potent RIPK1 inhibitor. RIPK1-IN-12 inhibits necroptosis in both human and mouse cells, with EC₅₀ values of 1.6 and 2.9 nM, respectively.

HY-160170

Necrosis inhibitor 3	Inhibitor
Necrosis inhibitor 3 (compound B3) is a poteng inhibitor of necrosis, with the IC₅₀ value of 0.29 nM in HT29 cells.

HY-116107

AG311	Inducer
AG311 is an anticancer and antimetastatic agent. AG311 induces rapid necrosis in numerous cancer cell lines.

HY-156920

VDX-111	Inducer
VDX-111 is an analog of vitamin D. VDX-111 exhibits cytotoxicity in ovarian cancer cells through upregulation of RIPK1/RIPK3 pathway and induction of necroptosis. VDX-111 promotes expressions of cytokines and exhibits antitumor activity in mouse model.

HY-155804

RIP1 kinase inhibitor 8	Inhibitor
RIP1 kinase inhibitor 8 (Compound 77) is a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor with an IC₅₀ of 20 nM. RIP1 kinase inhibitor 8 prevents necrotic cell death. RIP1 kinase inhibitor 8 shows a favorable pharmacokinetic profile in multiple species.

HY-156087

Cholicamideβ	Inducer
Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis.

HY-160169

Necrosis inhibitor 2	Inhibitor
Necrosis inhibitor 2 (Compound B19) is a cell necrosis inhibitor. Necrosis inhibitor 2 can be used to study diseases related to the necrosis pathway, including inflammation, tumors, metabolic diseases and neurodegenerative diseases.

HY-N10319R

Artepillin C (Standard)	Inducer
Artepillin C (Standard) is the analytical standard of Artepillin C (HY-N10319). This product is intended for research and analytical applications. Artepillin C is an orally active CREB/CRTC2 inhibitor and TRPA1 covalent agonist (EC₅₀=1.8 μM). Artepillin C inhibits CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression to regulate glucose and lipid metabolism. Artepillin C can also activate TRPA1 channels to induce spicy taste signals. Artepillin C can inhibit tumor cell proliferation, induce apoptosis, improve insulin resistance and inhibit liver lipid synthesis. Artepillin C can be used in the study of metabolic syndrome, tumor prevention and treatment, and inflammation.

HY-149052

SZM-1209	Inhibitor
SZM-1209 is an orally active, potent and specific RIPK1 inhibitor, with a K_d of 85 nM. SZM-1209 exhibits high anti-necroptotic activity (EC₅₀=22.4 ± 8.1 nM). SZM-1209 shows anti-SIRS (systemic inflammatory response syndrome), and anti-ALI (acute lung injury) effects.

HY-151541

MLKL-IN-3	Inhibitor
MLKL-IN-3 (compound 66) is a potent MLKL (Mixed lineage kinase domain-like protein) inhibitor. MLKL-IN-3 inhibits necroptosis in HT-29 cells and acts downstream of MLKL phosphorylation, with EC₅₀ of 31 nM. MLKL-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-W747676

Glyphosate-¹³C
Glyphosate-¹³C is the ¹³C-labeled Glyphosate (HY-B0863). Glyphosate, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders.

HY-173564

DW34	Inhibitor
DW34 is an orally active pan-BRD4-D1 biased inhibitor with additional BRD4-D2 inhibitive activity. DW34 displays comparable inhibitive efficacy to I-BET151 (HY-13235) (EC₅₀ = 0.16 μM) with low nanomolar EC₅₀ values of 0.14 μM. DW34 significantly reduces liver inflammation induced by LPS (HY-D1056) and APAP (HY-66005) via reducing chemokine expression and cellular necrosis.

HY-163390

RIP1 kinase inhibitor 9	Inhibitor
RIP1 kinase inhibitor 9 (compound SY-1) is a selective RIP kinase inhibitor. RIP1 kinase inhibitor 9 effectively suppresses the central inflammatory response induced by epilepsy. RIP1 kinase inhibitor 9 inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis in HT-29 cells with an EC₅₀ of 7.04 nM.

HY-W144308R

Tetrachlorohydroquinone (Standard)	Inducer
Tetrachlorohydroquinone (Standard) is the analytical standard of Tetrachlorohydroquinone (HY-W144308). This product is intended for research and analytical applications. Tetrachlorohydroquinone (TCHQ) is a metabolite of Pentachlorophenol. Tetrachlorohydroquinone induces reactive oxidant stress (ROS), inhibits apoptosis and induces necrosis in primary mouse splenocytes. Tetrachlorohydroquinone increases DNA lesions and induces oxidative stress in rodents.

HY-W013699R

Chlorhexidine diacetate (Standard)	Inducer
Chlorhexidine diacetate (Standard) is the analytical standard of Chlorhexidine diacetate (HY-W013699). This product is intended for research and analytical applications. Chlorhexidine diacetate is a orally active cationic antimicrobial agent that targets microbial cell membranes. Chlorhexidine diacetate binds to cell membrane phospholipids non-specifically, destroys membrane structure and induces leakage of cell contents. Chlorhexidine diacetate has broad-spectrum bactericidal activity against both Gram-positive and Gram-negative bacteria. Chlorhexidine diacetate can interfere with membrane permeability, cause protein precipitation and energy metabolism disorders, such as rapid inhibition of microbial growth and induction of cell death (necrosis or apoptosis).

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